Description
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.
Product information
CAS Number: 920650-00-6
Molecular Weight: 441.50
Formula: C22H23N3O5S
Chemical Name: N-[4-methoxy-3-(morpholine-4-sulfonyl)phenyl]-3-(1H-pyrrol-1-yl)benzamide
Smiles: COC1=CC=C(C=C1S(=O)(=O)N1CCOCC1)NC(=O)C1=CC=CC(=C1)N1C=CC=C1
InChiKey: IFXCVBOQNYHBMX-UHFFFAOYSA-N
InChi: InChI=1S/C22H23N3O5S/c1-29-20-8-7-18(16-21(20)31(27,28)25-11-13-30-14-12-25)23-22(26)17-5-4-6-19(15-17)24-9-2-3-10-24/h2-10,15-16H,11-14H2,1H3,(H,23,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (226.50 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 52 μM in the Alphascreen assay. NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells. NCGC00378430 (10 μM; 3 days) reverses the Sine oculis homeobox homolog 1 (SIX1)-induced increase in p-SMAD3 and does not alter total E-CAD levels. NCGC00378430 restores membranous E-CAD in MCF7-SIX1 cells, along with inhibiting FN1 expression. NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells). NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells.
In Vivo:
NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment. NCGC00378430 (20 mg/kg; IV) has a T1/2α of 0.25 hours.
Products are for research use only. Not for human use.
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